Development of rationally designed DNA N6 adenine methyltransferase inhibitors |
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| Authors: | Hobley Gerard McKelvie Jennifer C Harmer Jenny E Howe Jason Oyston Petra C F Roach Peter L |
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| Affiliation: | University of Southampton, School of Chemistry, University Road, Highfield, Southampton SO17 1BJ, UK. |
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| Abstract: | A series of bisubstrate inhibitors for DNA N6 adenine methyltransferase (Dam) have been synthesized by linking an amine analogue of S-adenosylmethionine to an aryl moiety designed to probe the binding pocket of the DNA adenine base. An initial structure-activity relationship study has identified substituents that increase inhibitor potency to the ～10 μM range and improve selectivity against the human cytosine methyltransferase Dnmt1. |
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